Target Information
Target General Information | Top | |||||
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Target ID |
T70539
(Former ID: TTDR00612)
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Target Name |
Melanin-concentrating hormone receptor 2 (MCHR2)
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Synonyms |
SLT; MCHR-2; MCH2R; MCH2 protein; MCH-R2; MCH-2R; MCH(2) receptor; MCH receptor 2; GPRv17; GPR145; G-protein coupled receptor 145; G protein coupled receptor 145
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Gene Name |
MCHR2
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Target Type |
Literature-reported target
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[1] | ||||
Function |
Receptor for melanin-concentrating hormone, coupled to G proteins that activate phosphoinositide hydrolysis.
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | ||||||
Sequence |
MNPFHASCWNTSAELLNKSWNKEFAYQTASVVDTVILPSMIGIICSTGLVGNILIVFTII
RSRKKTVPDIYICNLAVADLVHIVGMPFLIHQWARGGEWVFGGPLCTIITSLDTCNQFAC SAIMTVMSVDRYFALVQPFRLTRWRTRYKTIRINLGLWAASFILALPVWVYSKVIKFKDG VESCAFDLTSPDDVLWYTLYLTITTFFFPLPLILVCYILILCYTWEMYQQNKDARCCNPS VPKQRVMKLTKMVLVLVVVFILSAAPYHVIQLVNLQMEQPTLAFYVGYYLSICLSYASSS INPFLYILLSGNFQKRLPQIQRRATEKEINNMGNTLKSHF Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold |
Cell-based Target Expression Variations | Top | |||||
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Cell-based Target Expression Variations |
Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Human Similarity Proteins
Human Pathway Affiliation
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KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
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Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Affiliated Biological Pathways | Top | |||||
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Reactome | [+] 3 Reactome Pathways | + | ||||
1 | Peptide ligand-binding receptors | |||||
2 | G alpha (q) signalling events | |||||
3 | G alpha (i) signalling events | |||||
WikiPathways | [+] 4 WikiPathways | + | ||||
1 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
2 | GPCR ligand binding | |||||
3 | GPCR downstream signaling | |||||
4 | GPCRs, Other |
References | Top | |||||
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REF 1 | Identification and characterization of a second melanin-concentrating hormone receptor, MCH-2R. Proc Natl Acad Sci U S A. 2001 Jun 19;98(13):7564-9. | |||||
REF 2 | Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagoni... J Pharmacol Exp Ther. 2005 May;313(2):831-9. | |||||
REF 3 | Discovery and characterization of a potent and selective antagonist of melanin-concentrating hormone receptor 2. Bioorg Med Chem Lett. 2012 Jan 1;22(1):363-6. |
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